2. Protein Tyrosine Kinase/RTK
  3. FAK
    Pyk2
  4. PF-562271 besylate

PF-562271 besylate  (Synonyms: VS-6062 besylate)

Cat. No.: HY-10458 Purity: 99.17%
COA Handling Instructions

PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively.

For research use only. We do not sell to patients.

PF-562271 besylate Chemical Structure

PF-562271 besylate Chemical Structure

CAS No. : 939791-38-5

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 232 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 232 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 158 In-stock
Estimated Time of Arrival: December 31
10 mg USD 198 In-stock
Estimated Time of Arrival: December 31
50 mg USD 495 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of PF-562271 besylate:

Top Publications Citing Use of Products

    PF-562271 besylate purchased from MCE. Usage Cited in: Cell Death Dis. 2023 Feb 24;14(2):157.  [Abstract]

    PF-562271 (250 nM; 6 h) largely inhibits Akt-S6 phosphorylation in OE-MXRA5 priPC-1 cells.

    PF-562271 besylate purchased from MCE. Usage Cited in: Int J Cancer. 2015 Oct 1;137(7):1549-59.  [Abstract]

    786-O (a) and Caki-1 (b) are treated for 24 and 48h with increasing concentrations of PF-562,271 and adherent cells were counted. Cell lysates are evaluated through immunoblotting for total FAK following treatment for 24h.

    PF-562271 besylate purchased from MCE. Usage Cited in: Practical Oncology Journal. 2015, 29(5): 444-449.

    Effects and mechanism of Biglycan and FAK signaling pathway on the invasion and metastasis of colon cancer cells.

    PF-562271 besylate purchased from MCE. Usage Cited in: Cancer Res. 2013 May 1;73(9):2873-83.  [Abstract]

    FAK inhibition downregulates the AKT/mTOR pathway and CAS activity. A, protein levels measured by Western immunoblotting for AKT/mTOR pathway proteins in A673 and TC32 cells serum-starved overnight, treated with PF-562271 for 6 hours, and then stimulated with IGF-1 for 2 hours. Vinculin is used as the loading control. B, Western immunoblots showing downregulation of phospho-CAS but not phospho-ERK in A673 and TC32 cells after treatment with PF-562271.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively[1].

    IC50 & Target

    IC50: 1.5 nM (FAK), 13 nM (Pyk2), 30 nM (CDK2), 47 nM (CDK3), 58 nM (CDK1), 97 nM (CDK7), 97 nM (Flt3)[1]
    In Vitro

    PF-562271 (VS-6062) besylate is a 30- to 120-nM (15.2 to 60.1 ng/mL) inhibitor of cdk2/E, cdk5/p35, cdk1/B, and cdk3/E in recombinant enzyme assays[1]. PF-562,271 blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays[2]. Treatment of cells with PF-562,271 or knock-down of FAK by siRNA is observed to increase cell-cell adhesion strength[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    In Vivo

    PF-562,271 (33 mg/kg, p.o.) inhibits FAK phosphorylation in tumors in a dose- and time-dependent manner in tumor-bearing mice. FAK phosphorylation inhibition relative to total blood concentration of PF-562,271 results in a calculated EC50 of 93 ng/mL. PF-562,271 (25 mg/kg, p.o.) induces apoptosis 2-fold greater in treated tumors compared with vehicle-treated control tumors on day 3[1]. PF-562,271 (33 mg/kg, p.o.) and dasatinib extensively inhibit the movement of tumor cells in the animals. Inhibition of FAK kinase activity following treatment with PF-562,271 results in altered E-cadherin dynamics in vivo[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    665.66

    Appearance

    Solid

    Formula

    C27H26F3N7O6S2
    CAS No.
    SMILES

    CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O.O=S(C5=CC=CC=C5)(O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
    Solvent & Solubility
    In Vitro: 

    DMSO : 21.4 mg/mL (32.15 mM; Need ultrasonic and warming)

    H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5023 mL 7.5113 mL 15.0227 mL
    5 mM 0.3005 mL 1.5023 mL 3.0045 mL
    10 mM 0.1502 mL 0.7511 mL 1.5023 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 1.67 mg/mL (2.51 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 1.67 mg/mL (2.51 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 1.67 mg/mL (2.51 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.17%

    COA (254 KB) HNMR (209 KB) LCMS (252 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    Briefly, purified-activated FAK kinase domain (amino acid 410-689) is reacted with 50 μM ATP and 10 μg per well of a random peptide polymer of Glu and Tyr, p(Glu/Tyr), in kinase buffer [50 mM HEPES (pH 7.5), 125 mM NaCl, and 48 mM MgCl2] for 15 min. Phosphorylation of p(Glu/Tyr) is challenged with serially diluted compound at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is tested in triplicate. Phosphorylation of p(Glu/Tyr) is detected with a general antiphospho-tyrosine (PY20) antibody followed by horseradish peroxidase (HRP)-conjugated goat anti-mouse IgG antibody. HRP substrate is added, and absorbance readings at 450 nm are obtained after addition of stop solution (2mol/LH2SO4). IC50 values are determined using the Hill-Slope Model.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Exponentially growing cells are trypsinized and resuspended in sterile PBS and inoculated s.c. (1×106 cells per mouse in 200 μL) into the right flank of mice. Animals bearing tumors of appr 150 mm3 in size are divided into groups receiving either vehicle (5% Gelucire) or PF-562,271 (diluted in vehicle), and dosed by p.o. gavage. Animal body weight and tumor measurements are obtained every 2 d. Tumor volume (mm3) is measured with Vernier calipers and calculated. For all tumor growth inhibition experiments, 8 to 10 mice per dose group are used.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    PF-562271 besylate939791-38-5VS-6062 besylateFAKPyk2PTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseProline-rich tyrosine kinase 2Inhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Salutation

    Applicant Name *

    		 

    Email address *

    Phone number *

    		 

    Organization name *

    Department *

    		 

    Requested quantity *

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    PF-562271 besylate
    Cat. No.:
    HY-10458
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email address *

    Phone number

    		 

    Department *

    Organization name *

    		 

    Country or Region *

    Remarks

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.